The Werner Syndrome RecQ DNA helicase (WRN) plays a crucial role in DNA metabolism and genome stability. This patent collectively demonstrates the synthesis, composition and formulation about novel WRN inhibitors featuring bicyclic heterocycles for cancer treatment.
Provided herein are novel compounds as ARNT degraders, pharmaceutical compositions, use of such compounds in treating cancer, in particular, hematological cancer, and processes for preparing such compounds.
Provided herein are novel 6-aminopurine derivatives as POLQ inhibitors, pharmaceutical compositions, use of such compounds in treating cancer, and processes for preparing such compounds.
Provided herein are novel compounds as LPAR1 inhibitors, pharmaceutical compositions, use of such compounds in treating systemic sclerosis, and processes for preparing such compounds.
This patent describes novel substituted benzisoxazole sulfonamides as lysine acetyl transferase (KAT) inhibitors with potential applications in cancer therapy. It provides details on the synthesis of novel substituted benzisoxazole sulfonamides, their pharmaceutical composition, and the use in the treatment of cancers.
Provided herein are novel compounds as CX3CR1 modulators, pharmaceutical compositions, use of such compounds in treating cardiovascular diseases, and processes for preparing such compounds.
Drug patents are an important aspect of academic and industrial collaboration in drug discovery, including innovation of new drug candidates, the procedure of receiving granted patents of new drugs, and protecting them in the market and courts. The Microperspective considers various modes of collaboration between academics and industry: classic and nonclassic modes of academic patent licensing to the industry, academics used in patent litigations as expert witnesses, assessors, and amicus briefs.
Provided herein are novel imidazopyridazine compounds as IL-17 inhibitors, pharmaceutical compositions, use of such compounds in treating inflammatory diseases, and processes for preparing such compounds.
Provided herein are novel compounds as TREM2 agonists, pharmaceutical compositions, use of such compounds in treating Alzheimer’s disease, and processes for preparing such compounds.
Oxidative damage and cholinergic dysfunction are common pathological features of Alzheimer’s disease (AD). Maintaining the redox balance of neurons and cholinergic signaling through antioxidants and acetylcholinesterase (AChE) inhibition may provide therapeutic benefits for AD. In this regard, we discovered three AChE inhibitors with more potency than the positive control (rivastigmine; IC50 = 24.5 μM). Among these active compounds, C5 (a flavonoid derivative) was the most potent AChE inhibitor with an IC50 of 5.02 μM, followed by C1, C6, and C2 with IC50 values of 7.94 μM, 8.13 μM, and 27.52 μM, respectively. Compound C5 also demonstrated strong neuroprotective activity, rescuing PC12 cells from H2O2-induced damage and scavenging various ROS models. Interestingly, C5 also prevented memory impairments in the scopolamine-induced cognitive dysfunction zebrafish model. Our findings suggest that C5 is a potential drug lead for cholinergic dysfunction-related disorders such as AD.
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